Euphyllin ampoules 2.4% 5ml №10

Solution for intravenous administration

Composition

1 ml of solution for intravenous administration contains: aminophylline 24 mg, incl. theophylline 19.2 mg, ethylene diamine 4.8 mg.
Excipients: water for injections.

Packing

In 1 ampoule 5 ml (120 mg) solution. In the package 10 ampoules.

Mechanism of action

Euphyllin - a bronchodilator, PDE inhibitor. It is theophylline ethylene diamine salt (which facilitates solubility and increases absorption). It has a bronchodilator effect, apparently due to a direct relaxing effect on the smooth muscles of the respiratory tract and blood vessels of the lungs. It is believed that this action is caused by the selective inhibition of the activity of specific PDEs, which leads to an increase in the intracellular concentration of cAMP. The results of experimental studies in vitro show that the main role seems to play isoenzymes III and IV types. Suppression of the activity of these isoenzymes may also cause some side effects of aminophylline (theophylline), including vomiting, hypotension and tachycardia. Blocks adenosine (purine) receptors, which may be one of the factors of action on the bronchi.
Reduces airway hyperreactivity associated with the late phase of the reaction, caused by the inhalation of allergens, through an unknown mechanism that does not relate to the inhibition of PDE or to the blockade of the action of adenosine. There are reports that aminophylline increases the number and activity of T-suppressors in peripheral blood.
Increases mucociliary clearance, stimulates contraction of the diaphragm, improves the function of the respiratory and intercostal muscles, stimulates the respiratory center, increases its sensitivity to carbon dioxide and improves alveolar ventilation, which ultimately leads to a decrease in the severity and frequency of episodes of apnea. Normalizing the respiratory function, helps to saturate the blood with oxygen and reduce the concentration of carbon dioxide. Strengthens ventilation of the lungs in the conditions of a hypokalemia.
It has a stimulating effect on the activity of the heart, increases strength and heart rate, increases coronary blood flow and increases the need for oxygen in the myocardium. Reduces the tone of blood vessels (mainly vessels of the brain, skin and kidneys). It has a peripheral venodilating effect, reduces pulmonary vascular resistance, lowers pressure in the pulmonary circulation. Increases renal blood flow, has a moderate diuretic effect. Expands extrahepatic biliary tract. Stabilizes the membranes of mast cells, inhibits the release of mediators of allergic reactions. It inhibits platelet aggregation (inhibits platelet activating factor and PgE2α), increases erythrocyte resistance to deformation (improves the rheological properties of blood),reduces blood clots and normalizes microcirculation. It has a tocolytic effect, increases the acidity of gastric juice. In high doses, it has an epileptogenic effect.

- Asthmatic status (additional therapy).
- Apnea of ​​newborns.
- Disruption of cerebral circulation in ischemic type (as part of combination therapy).
- Left ventricular failure with bronchospasm and respiratory disorder by type of Cheyne-Stokes.
- Edematous syndrome of renal genesis (as part of complex therapy).
- Acute and chronic heart failure (as part of combination therapy).

Contraindications

- Severe arterial hyper - or hypotension.
- Tachyarrhythmias.
- Peptic ulcer of the stomach and duodenum in the acute phase.
- Hyperacid gastritis.
- Severe dysfunction of the liver and / or kidneys.
- Epilepsy.
- Hemorrhagic stroke.
- Retinal hemorrhage.
- Simultaneous use with ephedrine in children.
- Children's age (up to 3 years, for prolonged oral forms - up to 12 years).
- Hypersensitivity to aminophylline and theophylline.

Pregnancy and breastfeeding

Theophylline penetrates the placental barrier. The use of aminophylline during pregnancy can lead to the creation of potentially dangerous concentrations of theophylline and caffeine in the plasma of the newborn. Newborns whose mothers received aminophylline during pregnancy (especially in the third trimester) need medical supervision to control the possible symptoms of theophylline intoxication.
Theophylline is excreted in breast milk.When aminophylline is used in a lactating mother during lactation, irritability of the baby may occur.
Thus, the use of aminophylline during pregnancy and lactation (breastfeeding) is possible in cases where the intended benefit of therapy for the mother outweighs the potential risk to the fetus or child.

Dosage and administration

2.4% solution is injected into / in the jet.
Obstructive pulmonary disease
In the acute phase of adults:
The initial dose is 5-6 mg / kg (with a further increase in the dosage of the drug for every 0.5 mg / kg there is an increase in the concentration of aminophylline in the blood by 1 mcg / ml) it must be borne in mind that the concentration of aminophylline in the blood serum should not exceed 20 mcg / ml (possible development of side effects).
Maintenance dose - for smokers 4 mg / kg every 6 hours for non-smokers and patients with liver pathology - 2 mg / kg every 8 hours for children, the initial dose is 5-6 mg / kg. Supporting (in mg / kg) - calculated by the formula: children up to 6 months - 0.07 x age in weeks + 1.7 every 8 hours, children from 6 months to 1 year - 0.05 x age in weeks + 1, 25 every 6 hours, from 1 year to 9 years old - 5 mg / kg every 6 hours, from 9 to 12 years old - 4 mg / kg every 6 hours, from 12 to 16 years old - 3 mg / kg every 6 hours.
Out of aggravation to adults
The initial dose is 6-8 mg / kg / day (maximum 400 mg / day), divided into 3-4 doses with good tolerance, a further dose increase is possible by 25% every 2-3 days up to a maximum of 13 mg / kg / day (900 mg / kg / day).
Out of aggravation to children
Initial dose - 16 mg / kg / day (maximum 400 mg / day),divided into 3-4 doses with good tolerability, the dose can be increased by 25% every 2-3 days - up to the maximum daily dose, which is up to 1 year old - 0.3 x age in weeks + 8.0, from 1 year to 9 years old - 22 mg / kg, from 9 to 12 years old - 20 mg / kg, from 12 to 16 years old - 18 mg / kg, over 16 years old - 13 mg / kg.
With newborn apnea
The initial dose is 5 mg / kg (administered by nasogastric tube).
Maintenance dose - 2 mg / kg, in 2 doses. The course of treatment is several weeks, in rare cases - months.

Correction of the dosing regimen of aminophylline may be required for heart failure, abnormal liver function, chronic alcoholism, fever, acute respiratory disease.
Elderly patients may require a dose reduction.
When replacing the used dosage form of aminophylline to another, clinical observation and control of theophylline concentration in the blood plasma is necessary.
Do not use rectally in children.

Drug Interactions

With simultaneous use with sympathomimetics, mutual reinforcement of action occurs; with beta-blockers and lithium preparations - the action is mutually reduced. The intensity of the action of aminophylline may decrease (due to an increase in its clearance), while being used with phenobarbital, rifampicin, isoniazid, Carbamazepine, sulfinpyrazone, phenytoin, and also in smokers.
The intensity of the action of aminophylline may increase (due to a decrease in its clearance) with simultaneous use with macrolide antibiotics, Lincomycin, with quinolones, Allopurinol, beta-adrenergic blockers, cimetidine, disulfiram, fluvoxamine, hormonal oral contraceptives, isoprenaline, viloxazine, and for vaccination against influenza.
Xanthine derivatives can potentiate hypokalemia caused by the action of β 2 -adrenoreceptor stimulants, corticosteroids and diuretics.
Antidiarrheal drugs and enterosorbents reduce the absorption of aminophylline.
Pharmaceutical incompatible with acid solutions.

Symptoms: anorexia, diarrhea, nausea, vomiting, epigastric pain, Gastrointestinal bleeding, tachypnea, facial flushing, tachycardia, ventricular arrhythmias, insomnia, anxiety, photophobia, generalized convulsions.
Treatment: drug withdrawal, stimulation of its elimination from the body (gastric lavage, forced diuresis, hemosorption, plasmasorption, hemodialysis, peritoneal dialysis), symptomatic therapy.

Store in a dark place.

3 years